Effects of certain hallucinogenic amphetamine analogs on the release of [3H]-serotonin from rat brain synaptosomes
David E. Nichols, David Harley Lloyd, Andrew J. Hoffman, Maxine B. Nichols, G.k.w. Yim
Journal of Medicinal Chemistry May 1, 1982 DOI: 10.1021/jm00347a010 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Experimental study Peer reviewed |
|---|---|
| Population | Rat whole brain synaptosomes |
| Interventions | MDA PMA MDMA alpha-dimethylated derivatives |
| Dose | 1 and 10 micrometers |
| Topics | MDMA Serotonin |
| Keywords | Citation Amphetamine |
| Citations | 178 |
| Key findings | The (+) isomer of MDMA was more effective than the (-) isomer in inducing serotonin release at 1 micromolar, suggesting transmitter release may play a role in MDMA's biological activity. |
Abstract
The enantiomers of 3,4-(methylenedioxy)amphetamine (MDA), p-methoxyamphetamine (PMA), and N-Me-MDA (MDMA), along with their alpha, alpha-dimethylated derivatives, were evaluated for an effect on the release of [3H]serotonin from rat whole brain synaptosomes. The amphetamine isomers were all potent in inducing the release of [3H]serotonin at bath concentrations of 1 and 10 micrometers but were inactive at 0.1 micrometers. No significant difference in isomer potency was observed at the 10 micrometers concentration. However, at 1 micrometer the (+) isomer of MDMA was more effective in inducing release than was the (-) isomer. Since it is the (+) isomer which is clinically active, this result suggests that transmitter release may play a role in the biological activity of MDMA. By contrast, the alpha, alpha-dimethyl compounds were not effective in releasing serotonin, even at the highest bath concentration.